Head-to-head clinical analysis & difference comparison: details on mechanism of action, dosing, half-life, interactions, and maternal-fetal safety.
PROGRAF vs ELIDEL
Clinician-reviewed, head-to-head comparison of mechanism, dosing, pharmacokinetics, and safety profiles.
Last clinically reviewed: July 2026 · OpiCalc Medical Review Team
Calcineurin inhibitor; binds to FKBP-12, inhibits calcineurin, preventing dephosphorylation and nuclear translocation of NF-AT, thereby inhibiting T-cell activation and cytokine gene transcription.
Inhibits T-cell activation by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, thereby blocking cytokine transcription.
Prophylaxis of organ rejection in kidney, liver, and heart transplant recipients,Treatment of refractory acute cellular rejection after organ transplantation,Off-label: Severe atopic dermatitis, nephrotic syndrome, ulcerative colitis
Atopic dermatitis unresponsive to or intolerant of other topical treatments,Off-label: psoriasis, vitiligo, rosacea, contact dermatitis, lichen sclerosus, cutaneous lupus erythematosus
Initial oral dose: 0.1-0.15 mg/kg/day divided into 2 doses (every 12 hours). IV dose: 0.03-0.05 mg/kg/day as continuous infusion. Adjunct with corticosteroids.
Apply a thin layer of 1% cream to affected areas twice daily.
Terminal elimination half-life is approximately 8.7 hours (range 4-41 hours) in healthy volunteers; in liver transplant patients, half-life is approximately 11.7 hours (range 3.9-56 hours); prolonged in patients with hepatic impairment.
Terminal elimination half-life: 30–45 hours (mean 35 hours) following topical application; clinically, twice-daily dosing ensures therapeutic concentrations.
Primarily hepatic via CYP3A4 and CYP3A5; intestinal metabolism contributes. P-glycoprotein substrate.
Metabolized primarily by CYP3A4; major metabolite O-demethylated pimecrolimus.
Primarily fecal (approximately 92%) with biliary excretion as the major route; renal excretion accounts for about 2.4% of the dose as unchanged drug and metabolites.
Renal (negligible, <1% unchanged) and biliary/fecal (approximately 97% as metabolites); less than 1% of the dose is excreted renally as unchanged drug.
99% bound primarily to albumin and alpha-1-acid glycoprotein; also binds to erythrocytes and lipoproteins.
99% bound to plasma proteins (primarily albumin and alpha-1-acid glycoprotein).
Volume of distribution is approximately 0.99 L/kg (range 0.6-1.9 L/kg) in healthy subjects; higher values indicate extensive tissue distribution and binding to erythrocytes.
Vd ~ 10 L/kg (extensive tissue distribution); suggests significant extravascular binding and penetration into tissues.
Oral bioavailability is approximately 17-25% (range 4-89%) in transplant patients, with high inter- and intra-subject variability; absorption is influenced by food.
Topical: Systemic bioavailability is approximately 4% (range 1–7%) of applied dose; absorption increases with extent of skin lesion and thickness of application.
No specific GFR-based dose adjustment required, but monitor renal function closely due to nephrotoxicity. For severe renal impairment (Cr Cl <30 m L/min), reduce dose by 25-50% and monitor levels.
No dose adjustment required for any degree of renal impairment.
Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 25%. Child-Pugh C: reduce dose by 50% and titrate based on trough levels.
No formal studies in hepatic impairment; use caution in severe impairment.
Oral: 0.1-0.3 mg/kg/day divided every 12 hours. IV: 0.03-0.05 mg/kg/day continuous infusion. Monitor trough concentrations.
Apply a thin layer of 1% cream twice daily for children aged 2 years and older; not indicated for children under 2 years.
Start at lower end of dosing range due to potential age-related decline in renal function. Monitor renal function and tacrolimus levels closely.
No specific dose adjustment recommended; apply a thin layer of 1% cream twice daily as for adults.
Increased risk of lymphomas and other malignancies, particularly skin cancer; increased susceptibility to infections. Only should be prescribed by physicians experienced in immunosuppressive therapy.
Long-term safety of topical calcineurin inhibitors has not been established; rare cases of malignancy (e.g., lymphoma, skin cancer) have been reported; use should be limited to short-term and intermittent treatment.
Nephrotoxicity, neurotoxicity (tremor, headache, seizures), hypertension, hyperkalemia, hyperglycemia, thrombotic microangiopathy, risk of BK virus infection, increased risk of EBV-associated post-transplant lymphoproliferative disorder.
Increased risk of infections (e.g., eczema herpeticum, varicella zoster); avoid use on malignant or premalignant skin conditions; lymphadenopathy; photosensitivity; not recommended in patients with Netherton syndrome; potential for systemic immunosuppression; monitor for local irritation.
Hypersensitivity to tacrolimus or any component of the formulation, concomitant use with cyclosporine, and patients with or at risk for congenital long QT syndrome.
Hypersensitivity to pimecrolimus or any component of the formulation; history of malignancy; application to areas of active infection; Netherton syndrome; immunocompromised patients.
Grapefruit and grapefruit juice increase tacrolimus levels, avoid. High-fat meals may decrease absorption; take consistently with or without food. Avoid potassium-rich foods if hyperkalemia risk.
No known food interactions. Avoid grapefruit juice as it may increase drug levels (CYP3A4 inhibition).
Pregnancy Category C. Risk in first trimester: increased risk of congenital malformations (animal studies); human data limited. Second and third trimester: potential for fetal growth restriction, prematurity, and neonatal toxicity (hyperkalemia, renal dysfunction). Use only if benefit outweighs risk.
FDA Pregnancy Category C. Systemic exposure is minimal after topical application, but animal studies have shown developmental toxicity. No adequate human studies; risk cannot be excluded. Avoid in pregnancy unless clearly needed.
Excreted in breast milk; M/P ratio unknown. Weigh benefits of breastfeeding against potential risk of infant immunosuppression and renal toxicity. Consider avoiding or using alternative.
Not recommended. Pimecrolimus is excreted in milk in animal studies; unknown in humans. M/P ratio not available. Potential for serious adverse reactions in nursing infants.
Increased clearance and decreased bioavailability during pregnancy may necessitate higher doses; monitor trough concentrations frequently (every 1-2 weeks) and adjust to maintain therapeutic levels (typically 5-15 ng/m L for liver transplantation, adjust per indication). Increased dose requirements often seen in second and third trimesters.
No dose adjustment necessary; use minimal amount to control symptoms. Systemic absorption is negligible, so pharmacokinetic changes in pregnancy do not alter dosing.
Monitor trough levels 12 hours post-dose; target 5-20 ng/m L depending on organ. Avoid with live vaccines. Adjust dose for hepatic impairment. Cautious co-administration with nephrotoxic drugs. Grapefruit juice increases tacrolimus levels.
Topical calcineurin inhibitor for atopic dermatitis, reserved as second-line therapy for mild-to-moderate eczema due to boxed warning for rare malignancy risk. Apply thin layer only; avoid occlusive dressings. Do not use in immunocompromised patients. Intermittent use is recommended; continuous long-term use safety not established.
Take at the same time every day, 12 hours apart.,Do not eat grapefruit or drink grapefruit juice.,Report signs of infection, tremors, or changes in urine output.,Avoid live vaccines and limit sun exposure.,Do not stop abruptly; taper under medical supervision.
Apply only to affected skin areas; avoid eyes, mouth, and open wounds.,Use for short durations; do not use continuously for extended periods.,Avoid sun exposure and tanning beds; use sunscreen on treated areas.,Do not cover treated skin with bandages or wraps unless instructed.,Report any signs of infection, skin burning, or new skin growths to your doctor.,This drug is for external use only; wash hands after application unless treating hands.,Do not use if you have a weakened immune system or active skin infection.
No interactions on record
No interactions on record
Explore head-to-head clinical comparisons of other medications in the same therapeutic classes.
Common clinical questions about PROGRAF vs ELIDEL, answered by our medical review team.
PROGRAF is a Calcineurin Inhibitor that works by Calcineurin inhibitor; binds to FKBP-12, inhibits calcineurin, preventing dephosphorylation and nuclear translocation of NF-AT, thereby inhibiting T-cell activation and cytokine gene transcription.. ELIDEL is a Topical Calcineurin Inhibitor that works by Inhibits T-cell activation by binding to macrophilin-12 (FKBP-12) and inhibiting calcineurin, thereby blocking cytokine transcription.. They differ in pharmacokinetic profiles, FDA-approved indications, and side effect profiles.
Potency comparisons between PROGRAF and ELIDEL depend on the specific clinical indication. These are agents from distinct pharmacological classes and are not directly interchangeable by dose. A physician or clinical pharmacist should guide any therapeutic switching decisions.
The standard adult dose of PROGRAF is: Initial oral dose: 0.1-0.15 mg/kg/day divided into 2 doses (every 12 hours). IV dose: 0.03-0.05 mg/kg/day as continuous infusion. Adjunct with corticosteroids.. The standard adult dose of ELIDEL is: Apply a thin layer of 1% cream to affected areas twice daily.. Dosing should always be individualized based on indication, renal and hepatic function, age, and other patient factors.
No direct drug-drug interaction has been formally documented between PROGRAF and ELIDEL in current clinical databases. However, individual patient risk factors including other medications, organ function, and comorbidities should always be evaluated by a qualified healthcare provider.
The maternal-fetal safety profiles differ. PROGRAF is classified as Category C. Pregnancy Category C. Risk in first trimester: increased risk of congenital malformations (animal studies); human data limited. Second and third trimester: potential for fetal grow. ELIDEL is classified as Category C. FDA Pregnancy Category C. Systemic exposure is minimal after topical application, but animal studies have shown developmental toxicity. No adequate human studies; risk cannot be ex. Always consult a maternal-fetal medicine specialist before taking either drug during pregnancy or lactation.